Cannabinoids

<p>CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.</p>

<p>O-2050: strong CB1 antagonist (Ki 2.5 nM), CB2 inhibitor (Ki 0.2 nM); reduces mouse food intake, increases activity.</p>

<p>GW405833 hydrochloride, a potent and selective agonist of the cannabinoid-2 (CB2) receptor (EC 50 = 0.65 nM; maximum inhibition = 44.6%), exhibits significant antihyperalgesic effects in various rodent pain models [1] [2] [3].</p>

<p>2-Arachidonoyl glycerol (2-AG), a natural endocannabinoid ligand for the CB1 receptor, was isolated from porcine brain and characterized. Its congener, 2-linoleoyl glycerol (2-LG), which has a linoleoyl group instead of an arachidonoyl group, also exists alongside 2-AG in vivo. While 2-LG exhibits low intrinsic activity, it enhances the activity of 2-AG and other endocannabinoids through an "entourage" effect, attributed to the inhibition of breakdown and reuptake pathways that typically decrease endocannabinoid levels post-release.</p>

<p>(R)-Monlunabant ((R)-MRI-1891) serves as a CB1 receptor antagonist utilized in obesity and metabolic disease research [1].</p>

<p>MRL-650 is an oral, selective CB1 agonist; IC50: CB1=7.5 nM, CB2=4100 nM; anorexigenic effects noted.</p>

<p>Amauromine is a peripherally selective and potent cannabinoid receptor type 1 (CB1) receptor antagonist, a novel alkaloid with vasodilatory activity.</p>

<p>PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo.</p>

<p>Heptadecanoyl ethanolamide, an endogenous cannabinoid, serves as a synthetic analog of PEA, featuring an odd-numbered (17-carbon) fatty acid chain [1].</p>

<p>GW 833972A: selective CB2 agonist; reduces neural depolarization and citric acid cough in animals.</p>

<p>GP 1a: potent CB2 receptor agonist (EC50=7.1), 30x CB2 over CB1 preference, boosts P-ERK1/2, aids skin healing, anti-inflammatory.</p>

<p>Cannabichromevarin is a phytocannabinoid naturally found in very low levels compared to other cannabinoids from which it differs in having a propyl chain in place of a pentyl chain1. Based on its structure, it is believed to act as a potent anandamine inhibitor similarly to cannabichromene, however, the majority of its pharmacological and toxicological properties are currently unknown. In vitro assays have shown cannabichromevarin protect against oxidative stress in vitro in macrophages2. It was recently shown to be effective for treatment-resistant epilepsy in a patented combination with cannabidiol in a recent open-ended clinical trial3.</p>

<p>O-1269 acts as a partial agonist for the cannabinoid receptor 1 (CB1R), with a binding affinity (Ki) of 32 nM. Additionally, it exhibits analgesic properties.</p>

<p>MDA77 is a CB2 agonist with an EC50 value of 5.82 nM and exhibits no activity towards CB1.</p>

<p>FDU-PB-22, a novel synthetic cannabinoid, undergoes rapid metabolism in human liver microsomes (HLM) with a half-life of 12.4 minutes.</p>

<p>1'-Naphthoyl-2-methylindole (Compound 88) acts as a cannabinoid mimic and an inhibitor of Win 55212-2, displaying a 34% inhibition of [3H]Win 55212-2 binding to cannabinoid receptors at a concentration of 3 μM.</p>

<p>Potent CB1/2 agonist 1; crosses blood-brain barrier; anti-inflammatory, analgesic; for multiple sclerosis research.</p>

<p>AM8936: potent CB1 agonist, EC50 rCB1=8.6nM/hCB1=1.4nM, Ki rat CB1=0.55nM; potential for CNS, metabolic, pain, glaucoma research.</p>

<p>AB-FUBINACA 3-fluorobenzyl isomer is a synthetic cannabinoid and an indazole derivative, exhibiting high affinity for central CB1 receptors (Ki= 0.9 nM) and possessing anticonvulsant activity.</p>

<p>BAY 38-7271: potent neuroprotective, selective CB1/CB2 agonist, Ki of 1.85 nM (CB1) &amp; 5.96 nM (CB2).</p>